BPR1J-097 |
| Katalog-Nr.GC19080 |
BPR1J-097 ist ein neuartiger potenter FLT3-Inhibitor mit einem IC50 von 11nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1327167-19-0
Sample solution is provided at 25 µL, 10mM.
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BPR1J-097 is a novel potent FLT3 inhibitor with an IC50 of 11 nM.
References:
[1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81.
Kinase experiment: | The FLT3 Kinase-Glo kinase assays are carried out in 96-well plates at 30°C for 4 h in a final volume of 50 μL, including 25 mM Tris pH 7.4, 10 mM MgCl2, 4 mM MnCl2, 1 mM DTT, 0.02% Triton X-100, 0.01% BSA, 1 μM ATP, 20 μM peptide (GGMEDIYFEFMGGKKK), 75 ng recombinant FLT3 proteins, and test compound (BPR1J-097) at the indicated concentration. After incubation, 50 μL Kinase-Glo Plus Reagent is added and incubated at 25°C for 20 min. A 70 μL aliquot of each reaction mixture is transferred to a black microtiter plate and the luminescence is measured on a multilabel counter. Each IC50 value is determined by three different experiments[1]. |
Cell experiment: | Proliferation assays are performed by seeding 10 000 cells per well in a 96-well culture plate. After 16 h, cells are then treated with vehicle or BPR1J-097 Hydrochloride at various concentrations in medium for 72 h. Cell viability is quantitated using the MTS method. The results are determined by measuring absorbance at 490 nm using a plate reader. The GC50 value is defined as the amount of compound that causes 50% reduction in cell viability in comparison with DMSO-treated (vehicle) control and is calculated using Prism version 4 software[1]. |
Animal experiment: | Male nude mice of 8 weeks of age are used. Nude mice (n=5 to 7 per group) are inoculated subcutaneously with MOLM-13 (1×106 per flank) or MV4-11 cells (5×106 per flank). When the tumour size reaches 100 to 200 mm3, animals are grouped and treated with BPR1J-097 Hydrochloride at various doses in a 2-week treatment period as indicated. Animals are treated with BPR1J-097 Hydrochloride (10 and 25 mg/kg, i.v.) or vehicle as control at once daily for 5 days per week for 2 weeks. Tumour volumes are measured and calculated with the formula length×width2/2 after initiation of treatments. Tumour size and animal body weight are measured twice a week after tumour cell inoculation. At the end of the study, animals are killed by carbon dioxide inhalation followed by cervical dislocation[1]. |
References: [1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81. | |
| Cas No. | 1327167-19-0 | SDF | |
| Canonical SMILES | O=C(NC1=NNC(C2=CC=CC(NS(=O)(C3=CC=CC=C3)=O)=C2)=C1)C4=CC=C(N5CCN(C)CC5)C=C4 | ||
| Formula | C27H28N6O3S | M.Wt | 516.61 |
| Löslichkeit | DMSO : 6 mg/mL (10.85 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9357 mL | 9.6785 mL | 19.357 mL |
| 5 mM | 0.3871 mL | 1.9357 mL | 3.8714 mL |
| 10 mM | 0.1936 mL | 0.9678 mL | 1.9357 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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